• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

提高难吸收药物生物利用度的制剂策略,特别强调自乳化系统。

Formulation strategies to improve the bioavailability of poorly absorbed drugs with special emphasis on self-emulsifying systems.

作者信息

Gupta Shweta, Kesarla Rajesh, Omri Abdelwahab

机构信息

Department of Pharmaceutics, Parul Institute of Pharmacy, Limda, Waghodia, Vadodara, Gujarat 391760, India.

Department of Chemistry & Biochemistry, Laurentian University, 935 Ramsey Lake Road, Sudbury, ON, Canada P3E 2C6.

出版信息

ISRN Pharm. 2013 Dec 26;2013:848043. doi: 10.1155/2013/848043.

DOI:10.1155/2013/848043
PMID:24459591
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3888743/
Abstract

Poorly water-soluble drug candidates are becoming more prevalent. It has been estimated that approximately 60-70% of the drug molecules are insufficiently soluble in aqueous media and/or have very low permeability to allow for their adequate and reproducible absorption from the gastrointestinal tract (GIT) following oral administration. Formulation scientists have to adopt various strategies to enhance their absorption. Lipidic formulations are found to be a promising approach to combat the challenges. In this review article, potential advantages and drawbacks of various conventional techniques and the newer approaches specifically the self-emulsifying systems are discussed. Various components of the self-emulsifying systems and their selection criteria are critically reviewed. The attempts of various scientists to transform the liquid self-emulsifying drug delivery systems (SEDDS) to solid-SEDDS by adsorption, spray drying, lyophilization, melt granulation, extrusion, and so forth to formulate various dosage forms like self emulsifying capsules, tablets, controlled release pellets, beads, microspheres, nanoparticles, suppositories, implants, and so forth have also been included. Formulation of SEDDS is a potential strategy to deliver new drug molecules with enhanced bioavailability mostly exhibiting poor aqueous solubility. The self-emulsifying system offers various advantages over other drug delivery systems having potential to solve various problems associated with drugs of all the classes of biopharmaceutical classification system (BCS).

摘要

水溶性差的候选药物正变得越来越普遍。据估计,大约60%-70%的药物分子在水性介质中的溶解度不足,和/或渗透性非常低,以至于口服给药后无法从胃肠道(GIT)充分且可重复地吸收。制剂科学家必须采用各种策略来提高它们的吸收。脂质体制剂被认为是应对这些挑战的一种有前景的方法。在这篇综述文章中,讨论了各种传统技术以及更新的方法(特别是自乳化系统)的潜在优缺点。对自乳化系统的各种成分及其选择标准进行了严格审查。还包括了各位科学家通过吸附、喷雾干燥、冻干、熔融制粒、挤出等方法将液体自乳化药物递送系统(SEDDS)转变为固体SEDDS,以制备各种剂型,如自乳化胶囊、片剂、控释微丸、珠子、微球、纳米颗粒、栓剂、植入剂等的尝试。SEDDS的制剂是一种潜在的策略,可用于递送生物利用度提高的新药分子,这些分子大多表现出水溶性差的问题。与其他药物递送系统相比,自乳化系统具有多种优势,有可能解决与生物药剂学分类系统(BCS)所有类别药物相关的各种问题。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd73/3888743/edb69a9d7ac3/ISRN.PHARMACEUTICS2013-848043.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd73/3888743/75c684f13098/ISRN.PHARMACEUTICS2013-848043.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd73/3888743/edb69a9d7ac3/ISRN.PHARMACEUTICS2013-848043.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd73/3888743/75c684f13098/ISRN.PHARMACEUTICS2013-848043.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd73/3888743/edb69a9d7ac3/ISRN.PHARMACEUTICS2013-848043.002.jpg

相似文献

1
Formulation strategies to improve the bioavailability of poorly absorbed drugs with special emphasis on self-emulsifying systems.提高难吸收药物生物利用度的制剂策略,特别强调自乳化系统。
ISRN Pharm. 2013 Dec 26;2013:848043. doi: 10.1155/2013/848043.
2
Spray Drying as an Effective Method in the Development of Solid Self- Emulsifying Drug Delivery Systems.喷雾干燥法在固体自乳化药物传递系统开发中的应用。
Curr Drug Deliv. 2023;20(5):508-525. doi: 10.2174/1567201819666220516103042.
3
Preparation and evaluation of Vinpocetine self-emulsifying pH gradient release pellets.长春西汀自乳化pH梯度释放微丸的制备与评价
Drug Deliv. 2017 Nov;24(1):1598-1604. doi: 10.1080/10717544.2017.1388453.
4
Development and Evaluation of Liquid and Solid Self-Emulsifying Drug Delivery Systems for Atorvastatin.阿托伐他汀液体和固体自乳化药物递送系统的开发与评价
Molecules. 2015 Nov 25;20(12):21010-22. doi: 10.3390/molecules201219745.
5
Overview of solidification techniques for self-emulsifying drug delivery systems from industrial perspective.从工业角度概述自乳化药物传递系统的固化技术。
Int J Pharm. 2017 Nov 30;533(2):335-345. doi: 10.1016/j.ijpharm.2017.05.036. Epub 2017 May 18.
6
A Rundown Through Various Methods Used in the Formulation of Solid Self-Emulsifying Drug Delivery Systems (S-SEDDS).各种用于制备固体自乳化药物传递系统(S-SEDDS)的方法概述。
AAPS PharmSciTech. 2019 Oct 25;20(8):323. doi: 10.1208/s12249-019-1550-5.
7
A Comprehensive Insight on Recent Advancements in Self-emulsifying Drug Delivery Systems.自乳化药物传递系统的最新进展综述
Curr Drug Deliv. 2023;20(8):1095-1114. doi: 10.2174/1567201819666220914113324.
8
Self-emulsifying drug delivery systems: a novel approach to deliver drugs.自乳化药物传递系统:一种新的药物传递方法。
Drug Deliv. 2022 Dec;29(1):1811-1823. doi: 10.1080/10717544.2022.2083724.
9
Self-emulsifying Drug Delivery System Improve Oral Bioavailability: Role of Excipients and Physico-chemical Characterization.自乳化药物传递系统提高口服生物利用度:辅料的作用和物理化学特征。
Pharm Nanotechnol. 2020;8(4):290-301. doi: 10.2174/2211738508666200811104240.
10
Self-emulsifying drug delivery systems (SEDDS): formulation development, characterization, and applications.自乳化药物传递系统(SEDDS):制剂开发、特性描述和应用。
Crit Rev Ther Drug Carrier Syst. 2009;26(5):427-521. doi: 10.1615/critrevtherdrugcarriersyst.v26.i5.10.

引用本文的文献

1
PROTAC Delivery Strategies for Overcoming Physicochemical Properties and Physiological Barriers in Targeted Protein Degradation.用于克服靶向蛋白质降解中物理化学性质和生理屏障的PROTAC递送策略
Pharmaceutics. 2025 Apr 9;17(4):501. doi: 10.3390/pharmaceutics17040501.
2
Phytosomes-unraveling the Unique Properties of Plant-derived Nanotechnological Drug Delivery Systems: A Review.植物脂质体——解析植物源纳米技术药物递送系统的独特性质:综述
Curr Med Chem. 2025 Jan 24. doi: 10.2174/0109298673319759250116104648.
3
Enhancing drug solubility through competitive adsorption on silica nanosurfaces with ultrahigh silanol densities.

本文引用的文献

1
Porous polystyrene beads as carriers for self-emulsifying system containing loratadine.多孔聚苯乙烯珠粒作为含氯雷他定自乳化系统的载体
AAPS PharmSciTech. 2006 Mar;7(1):E199-E205. doi: 10.1208/pt070128. Epub 2017 Mar 8.
2
Self-nanoemulsifying drug delivery system of glimepiride: design, development, and optimization.格列美脲自纳米乳化药物递送系统:设计、开发与优化。
PDA J Pharm Sci Technol. 2013 May-Jun;67(3):201-13. doi: 10.5731/pdajpst.2013.00914.
3
Development of docetaxel-loaded solid self-nanoemulsifying drug delivery system (SNEDDS) for enhanced chemotherapeutic effect.
通过在具有超高硅醇密度的二氧化硅纳米表面上进行竞争性吸附来提高药物溶解度。
Proc Natl Acad Sci U S A. 2025 Jan 28;122(4):e2423426122. doi: 10.1073/pnas.2423426122. Epub 2025 Jan 23.
4
Health Benefits of Epigallocatechin Gallate and Forskolin with a Special Emphasis on Glaucoma and Other Retinal Diseases.表没食子儿没食子酸酯和毛喉素对健康的益处,特别关注青光眼和其他视网膜疾病。
Medicina (Kaunas). 2024 Nov 27;60(12):1957. doi: 10.3390/medicina60121957.
5
Nanotechnology in Drug Delivery: Anatomy and Molecular Insight into the Self-Assembly of Peptide-Based Hydrogels.药物递送中的纳米技术:基于肽的水凝胶自组装的剖析与分子洞察
Molecules. 2024 Nov 29;29(23):5654. doi: 10.3390/molecules29235654.
6
Hypocrellin: A Natural Photosensitizer and Nano-Formulation for Enhanced Molecular Targeting of PDT of Melanoma.竹红菌素:一种天然光敏剂和纳米制剂,可增强 PDT 对黑色素瘤的分子靶向。
Wiley Interdiscip Rev Nanomed Nanobiotechnol. 2024 Nov-Dec;16(6):e1997. doi: 10.1002/wnan.1997.
7
Development and Evaluation of a Cost-Effective, Carbon-Based, Extended-Release Febuxostat Tablet.开发和评估一种经济实惠、基于碳的、延长释放的非布司他片剂。
Molecules. 2024 Sep 29;29(19):4629. doi: 10.3390/molecules29194629.
8
Innovative Bedaquiline-Based Delivery Systems for Multidrug-Resistant Tuberculosis Treatment.用于耐多药结核病治疗的基于贝达喹啉的创新给药系统。
Infect Disord Drug Targets. 2025;25(4):e18715265318306. doi: 10.2174/0118715265318306240816104553.
9
Unveiling the Preparation and Characterization of Lercanidipine Hydrochloride in an Oral Solid Self-Nanoemulsion for Enhancing Oral Delivery.揭示用于增强口服给药的盐酸乐卡地平口服固体自纳米乳剂的制备与表征
Cureus. 2024 Jul 13;16(7):e64468. doi: 10.7759/cureus.64468. eCollection 2024 Jul.
10
Neuroprotective efficiency of celecoxib vesicular bilosomes for the management of lipopolysaccharide-induced Alzheimer in mice employing 2 full factorial design.采用 2 全因子设计评估塞来昔布囊泡双分子层用于治疗脂多糖诱导的阿尔茨海默病的神经保护效率。
Inflammopharmacology. 2024 Dec;32(6):3925-3942. doi: 10.1007/s10787-024-01522-y. Epub 2024 Jul 17.
载多西紫杉醇固体自乳化药物传递系统(SNEDDS)的研制及其增强化疗效果。
Int J Pharm. 2013 Aug 16;452(1-2):412-20. doi: 10.1016/j.ijpharm.2013.05.034. Epub 2013 May 22.
4
Proposal of stability categories for nano-dispersions obtained from pharmaceutical self-emulsifying formulations.从药剂学自乳化制剂中获得的纳米分散体的稳定性分类建议。
Int J Pharm. 2013 Mar 25;446(1-2):70-80. doi: 10.1016/j.ijpharm.2013.02.005. Epub 2013 Feb 10.
5
Enhanced dissolution of celecoxib by supersaturating self-emulsifying drug delivery system (S-SEDDS) formulation.通过超饱和自乳化药物传递系统(S-SEDDS)制剂增强塞来昔布的溶解。
Arch Pharm Res. 2013 Jan;36(1):69-78. doi: 10.1007/s12272-013-0011-z.
6
Supersaturated self-nanoemulsifying drug delivery systems (Super-SNEDDS) enhance the bioavailability of the poorly water-soluble drug simvastatin in dogs.超饱和自微乳药物传递系统(Super-SNEDDS)提高了犬体内难溶性药物辛伐他汀的生物利用度。
AAPS J. 2013 Jan;15(1):219-27. doi: 10.1208/s12248-012-9433-7. Epub 2012 Nov 21.
7
Development and characterization of solid lipid nanoparticles for enhancement of oral bioavailability of Raloxifene.用于提高雷洛昔芬口服生物利用度的固体脂质纳米粒的研制与表征
J Pharm Bioallied Sci. 2012 Mar;4(Suppl 1):S14-6. doi: 10.4103/0975-7406.94121.
8
Optimized nanoemulsifying systems with enhanced bioavailability of carvedilol.优化的纳米乳剂系统可提高卡维地洛的生物利用度。
Colloids Surf B Biointerfaces. 2013 Jan 1;101:465-74. doi: 10.1016/j.colsurfb.2012.07.017. Epub 2012 Jul 21.
9
Identification and molecular interpretation of the effects of drug incorporation on the self-emulsification process using spectroscopic, micropolarimetric and microscopic measurements.利用光谱、微偏振和显微镜测量,鉴定和分子解释药物掺入对自乳化过程的影响。
Mol Pharm. 2012 Sep 4;9(9):2658-68. doi: 10.1021/mp300219h. Epub 2012 Aug 22.
10
Modification of physicochemical characteristics of active pharmaceutical ingredients and application of supersaturatable dosage forms for improving bioavailability of poorly absorbed drugs.改善难吸收药物生物利用度的活性药物成分理化性质修饰及超饱和剂型的应用。
Adv Drug Deliv Rev. 2012 May 1;64(6):480-95. doi: 10.1016/j.addr.2011.10.009. Epub 2012 Jan 13.